Hemmati Khadijeh, Ghaemy Mousa
Polymer Research Laboratory, Faculty of Chemistry, University of Mazandaran, Babolsar, Iran.
Polymer Research Laboratory, Faculty of Chemistry, University of Mazandaran, Babolsar, Iran.
Int J Biol Macromol. 2016 Jun;87:415-25. doi: 10.1016/j.ijbiomac.2016.03.005. Epub 2016 Mar 5.
In this study, new pH/temperature responsive graft copolymers were synthesized based on natural Tragacanth Gum (TG) carbohydrate and their controlled drug release was investigated. Amphiphilic alkyne terminated terpolymers (mPEG-PCL-PDMAEMA-CCH)s consist of methylated poly(ethyleneglycol) (mPEG), polycaprolactone (PCL), and poly(dimethylaminoethylmethacrylate) (PDMAEMA) were synthesized by using ring opening polymerization (ROP) and atom transfer radical polymerization (ATRP), and then were grafted onto azide-functionalized TG molecules by click chemistry. Different techniques such as FT-IR, (1)H NMR, gel permeation chromatography (GPC), thermo-gravimetrical analysis (TGA) and scanning electron microscopy (SEM) were used to verify the successful synthesis of graft copolymers (TG-g-PDMAEMA-PCL-mPEG)s. The graft copolymers self-assembled to single micelles in aqueous solution and upon pH changes further assembled into micellar aggregates. These micelles were used to prepare quercetin loaded nanocarriers by probe sonication method. Size and morphology of the nanocarriers were studied by dynamic light scattering (DLS) and SEM. The in vitro release behavior of quercetin from these micelles showed pH-dependence. The results showed that release profile of quercetin best followed the first order model.
在本研究中,基于天然刺梧桐胶(TG)碳水化合物合成了新型pH/温度响应性接枝共聚物,并对其控释性能进行了研究。两亲性炔基封端的三元共聚物(mPEG-PCL-PDMAEMA-CCH)由甲基化聚乙二醇(mPEG)、聚己内酯(PCL)和聚(甲基丙烯酸二甲氨基乙酯)(PDMAEMA)组成,通过开环聚合(ROP)和原子转移自由基聚合(ATRP)合成,然后通过点击化学接枝到叠氮官能化的TG分子上。采用傅里叶变换红外光谱(FT-IR)、核磁共振氢谱(1H NMR)、凝胶渗透色谱(GPC)、热重分析(TGA)和扫描电子显微镜(SEM)等不同技术来验证接枝共聚物(TG-g-PDMAEMA-PCL-mPEG)的成功合成。接枝共聚物在水溶液中自组装成单分子胶束,并在pH值变化时进一步组装成胶束聚集体。通过探针超声法使用这些胶束制备了载槲皮素的纳米载体。通过动态光散射(DLS)和SEM研究了纳米载体的尺寸和形态。槲皮素从这些胶束中的体外释放行为显示出pH依赖性。结果表明,槲皮素的释放曲线最符合一级模型。